Found 7 hits in this display Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
A disintegrin and metalloproteinase with thrombospondin motifs 6
(Human) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 12.5 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |
A disintegrin and metalloproteinase with thrombospondin motifs 5
(Homo sapiens (Human)) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 12.5 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE IX: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by human ADAMTS-5.For th... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |
ADAMTS5
(Rattus norvegicus (Rat)) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | PDB
UniProtKB/TrEMBL
GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 12.5 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE VII: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by rnADAMTS-5 (1-564-6H... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |
A disintegrin and metalloproteinase with thrombospondin motifs 4
(Homo sapiens (Human)) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 37.5 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE VI: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by human ADAMTS4.For the... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |
Matrix metalloproteinase-14
(Homo sapiens (Human)) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE XIII: The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat #AS-27076) by human MMP13 (Enzo Life Scien... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |
Collagenase 3
(Homo sapiens (Human)) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | PDB MMDB
NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE XII: The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat #AS-27076) by human MMP13 (Chemicon, Cat #C... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |
Disintegrin and metalloproteinase domain-containing protein 17
(Homo sapiens (Human)) | BDBM471793
(5-[3-[(3S)-4-(3,4- difluoro-5- methoxy-phenyl)- 3-...)Show SMILES COc1cc(cc(F)c1F)N1CCN(C[C@@H]1C)C(=O)[C@@H](C)C[C@@]1(C)NC(=O)NC1=O |r| Show InChI InChI=1S/C20H26F2N4O4/c1-11(9-20(3)18(28)23-19(29)24-20)17(27)25-5-6-26(12(2)10-25)13-7-14(21)16(22)15(8-13)30-4/h7-8,11-12H,5-6,9-10H2,1-4H3,(H2,23,24,28,29)/t11-,12-,20+/m0/s1 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
GALAPAGOS NV
US Patent
| Assay Description TABLE XI: The basis for the assay is the cleavage of the substrate 5FAM-LAQAVRSSSRK-5TAMRA (SEQ ID NO: 3) (Anaspec, custom 34891) by human TACE (R&D ... |
US Patent US10829478 (2020)
BindingDB Entry DOI: 10.7270/Q2X351H2 |
More data for this Ligand-Target Pair | |